Dynamic phase behavior of amorphous solid dispersions revealed with in situ stimulated Raman scattering microscopy
This study reports the application of in situ stimulated Raman scattering (SRS) microscopy for real-time chemically-specific imaging of dynamic phase phenomena in amorphous solid dispersions (ASD). Using binary ritonavir and poly(vinylpyrrolidone-vinyl acetate) films with different drug loadings (0-100% w/w) as model systems, we employed SRS…
Studies on the in vitro ion exchange kinetics and thermodynamics and in vivo pharmacokinetics of the…
The short half-life and bitter taste of carbinoxamine maleate (CAM) lead to poor compliance by pediatric patients who are being treated for allergic rhinitis. To address these issues, carbinoxamine-resin complexes (CRCs) were prepared by…
Underpinning mechanistic understanding of the segregation phenomena of pharmaceutical blends using a…
The segregation of an active pharmaceutical ingredient (API) within a powder blend is one of the major manufacturing obstacles in achieving content uniformity. Segregation can be due to differences in physicochemical properties of…
Continuous twin screw granulation: Robustness of lactose/MCC-based formulations
In recent years, significant progress has been made in the field of continuous twin screw granulation. However, only limited knowledge is currently available on the impact of active pharmaceutical ingredient (API) properties on granule…
Functionalised calcium carbonate as a coformer to stabilize amorphous drugs by mechanochemical…
The aim of this study was to investigate the amorphization, physical stability and drug release of a model drug, carvedilol (CAR), when loaded onto functionalised calcium carbonate (FCC) using mechanochemical activation (vibrational ball…
In-situ forming implants for dual controlled release of chlorhexidine and ibuprofen for…
In-situ forming implants (ISFI) which simultaneously release an antimicrobial and anti-inflammatory drug in a controlled manner offer an interesting potential for local periodontitis treatment. In this study, poly(lactic-co-glycolic acid)…
Enhancing Oral Bioavailability of Apigenin Using a Bioactive Self-Nanoemulsifying Drug Delivery…
Apigenin (APG) is a very well-known flavonoid for its anti-inflammatory and anticancer properties. The purpose of this study is to improve the solubility and bioavailability of APG using a stable bioactive self-nanoemulsifying drug delivery…
Development and evaluation of solid dispersion based rapid disintegrating tablets of poorly…
Glimepiride is an effective oral hypoglycemic agent that lowers the glucose level of blood by stimulating insulin release from beta cells of the pancreas. However, the poor aqueous solubility (i.e., <0.004 mg/ml) and wettability of drugs…
Spray dried VSV-vectored vaccine is thermally stable and immunologically active in vivo
Effective vaccine delivery and coverage to rural and resource-poor countries is hindered by the dependence on cold chain storage. As such, developments of cold chain-free technologies are highly sought. Although spray dried adenoviral…
Microemulsion assisted transdermal delivery of a hydrophilic anti-osteoporotic drug: Formulation, in…
Gastrointestinal adverse effects such as esophageal irritation and ulcers are the major disadvantages of the oral administration of alendronate (ALD) and nitrogen-containing bisphosphonate. We hypothesized that the transdermal delivery of…
Rebaudioside A/TPGS mixed nanomicelles as promising nanocarriers for nimodipine ocular delivery
Nimodipine (NMD), a calcium channel blocker, has demonstrated benefits in treating glaucoma. However, its ocular therapeutic application remains limited due to its poor aqueous solubility, which restrains the development of an ophthalmic…
Accelerated Aqueous Solubility and Antibacterial Activity of Cefuroxime Axetil Using…
This investigation was undertaken to enhance the solubility and consequent antibacterial activity of cefuroxime axetil (CA), a β-lactamase-stable broad spectrum second generation cephalosporin through solid dispersion (SD) technique. For…
The Interplay Between Liver First-Pass Effect and Lymphatic Absorption of Cannabidiol and Its…
For highly lipophilic drugs, passage into the intestinal lymphatic system rather than the portal vein following oral administration may represent a major alternative route of delivery into the general circulation. Increasing intestinal…
Spontaneous In Situ Formation of Liposomes from Inert Porous Microparticles for Oral Drug Delivery
Despite the wide-spread use of liposomal drug delivery systems, application of these systems for oral purposes is limited due to their large-scale formulation and storage issues. Proliposomes are one of the formulation approaches for…
DLP 3D Printing Meets Lignocellulosic Biopolymers: Carboxymethyl Cellulose Inks for 3D Biocompatible…
The development of new bio-based inks is a stringent request for the expansion of additive manufacturing towards the development of 3D-printed biocompatible hydrogels. Herein, methacrylated carboxymethyl cellulose (M-CMC) is investigated as…
Eutectic mixtures as an approach to enhance solubility, dissolution rate and oral bioavailability of…
Eutectic mixtures have been known for a long time in the pharmaceutical field. However, its potential as a system to improve the solubility and dissolution of poorly water-soluble drugs remains little explored. Studies involving the…
Investigation into the Stability, Crystallization Kinetics, and Heating Rate Dependent…
Poor aqueous solubility is a major challenge for formulation scientists as more than 40% of new chemical entities developed in the pharmaceutical industry are insoluble in water. The high energy amorphous form offers enhanced solubility and…
Friday’s Top 5 by pharmaexcipients
Another week full of great scientific publications - find the one you liked most! Top post of the last 30 days is still "How to improve API Bioavailability?"as you can also see in the Top post of 2020.
Top posts of the week
#1…
Chinese Excipient DMF
Since January 1, 2018, CFDA has not been accepting Active Pharmaceutical Ingredients (APIs), Pharmaceutical Excipients and Pharmaceutical Packaging Materials registration application independently. The Active Pharmaceutical Ingredients…
Preparation, characterization and improved release profile of ibuprofen-phospholipid association
Ibuprofen is a widely prescribed non-steroidal and anti-inflammatory drug, which is practically insoluble in water and causes gastrointestinal (GI) side effects. Ibuprofen-phosphathidylcholine association (IPA) was prepared by refluxing…
Role of excipients in amorphous solid dispersions
Solid dispersions – a great way to increase the solubility and bioavailability of your drug
In a solid dispersion the drug is dispersed in a carrier with the system appearing to be in a solid state. Target is an increase in solubility and…
Incompatibility Check with ZoomLab™ – latest update of the Formulation Wizard
The updated formulation wizard in ZoomLab™ 1.4 includes an incompatibility check. You can predict potential incompatibilities between active ingredients and excipients. Incompatibilities include:
Ionic interactions
Hydrolysis…
Liquisolid Technique: a Novel Tool to Develop Aceclofenac-Loaded Eudragit L-100 and RS-100-Based…
One of the main problems with NSAIDs is the dosing frequency, which leads to patients’ noncompliance. To overcome this, fabrication of sustained release formulation of the drug is considered a well-reputed technique. The present study aimed…
Nanomedicine and Chemotherapeutics Drug Delivery: Challenges and Opportunities
Cancer is considered as one of the biggest threats to human worldwide. Researchers suggest that tumour is not just a single mass, it comprises cancerous cells surrounded by noncancerous cells such as immune cells, adipocytes, and cancer…
Robustness Optimization of an Existing Tablet Coating Process Applying Retrospective Knowledge…
The objective of these studies is to verify and validate the improvement in the inter-tablet coating uniformity for an industrially commercialized coated tablet, without involving changes in the approved registration dossier. Using the CPP…
A Novel Oral Syringe for Dosing and Administration of Multiparticulate Formulations: Acceptability…
The popularity of multiparticulate formulations (MPs) as a paediatric dosage form continues to increase. MPs comprise of multiple small units that are easy-to-swallow. Currently, MPs are commonly manufactured into unit doses that are either…
Accordion Pill®: Laminated, folded, encapsulated
So much for capsules can only be filled with powders, pellets, microtablets or liquids! The Accordion Pill® by Intec Pharma Ltd. is a drug delivery system that uses active ingredient containing polymeric films, which are folded into an…
Supercritical Antisolvent Process for Pharmaceutical Applications: A Review
The supercritical antisolvent (SAS) technique has been widely employed in the biomedical field, including drug delivery, to obtain drug particles or polymer-based systems of nanometric or micrometric size. The primary purpose of producing…
Impact of nanoparticle size and solid state on dissolution rate by investigating modified drug…
Nanoparticles with reduced crystallinity are normally produced by bottom-up (precipitation) processes; however, the drug loading can be limited. The objective was to generate such nanoparticles using modified drugs coupled with high…
Acceptability in the Older Population: The Importance of an Appropriate Tablet Size
Presenting many advantages, solid oral dosage forms (SODFs) are widely manufactured and frequently prescribed in older populations regardless of the specific characteristics of patients. Commonly, patients with dysphagia (swallowing…
Hot-Melt 3D Extrusion for the Fabrication of Customizable Modified-Release Solid Dosage Forms
In this work, modified-release solid dosage forms were fabricated by adjusting geometrical properties of solid dosage forms through hot-melt 3D extrusion (3D HME). Using a 3D printer with air pressure driving HME system, solid dosage forms…
Tinctures or oily solutions for CBD
Tinctures, as oily solutions, are an ancient mode of preparation of plant extracts, but are still very actual and attractive, especially for cannabinoid formulations. With a straightforward development, they can easily be developed. They…
The impact of the degree of intimate mixing on the compaction properties of materials produced by…
Direct compression remains one of the most favourable methods available to produce tablet compacts due to its simplicity, efficiency and cost effectiveness however, the technique still remains unsuitable for the majority of formulations due…
The EsoCap-system – An innovative platform to drug targeting in the esophagus
For the therapy of esophageal diseases such as eosinophilic esophagitis, there are no possibilities of local targeted therapy. This publication describes a novel, innovative drug delivery concept, that enables a targeted, long-lasting…
Amorphous solid dispersion dry powder for pulmonary drug delivery: Advantages and challenges
Amorphous solid dispersion (ASD) is commonly used in pharmaceutical industry. It has been mainly employed to enhance the oral bioavailability of poorly water-soluble drugs that belong to class II and IV of the biopharmaceutical…